Cyclic guanidines. XV. Synthesis and biological activities of (substituted phenyl)-imidazo(1,2-a)imidazole derivatives.
作者:FUMIYOSHI ISHIKAWA、MASAYUKI KITAGAWA、YOSHINARI SATOH、JUNJI SAEGUSA、SATORU TANAKA、SEIICHI SHIBAMURA、TOMOMI CHIBA
DOI:10.1248/cpb.33.2838
日期:——
A series of (substituted phenyl)-2, 3, 5, 6-tetrahydro-1H-imidazo [1, 2-a] imidazoles (10) and their 2- or 3-oxo derivatives (20 and 21) were unambiguously prepared. These compounds were evaluated for antihypertensive and diuretic activities. Antihypertensive activity in spontaneously hypertensive rats (SHR) was observed in the series of compounds 10, whereas compounds 20 and 21 did not possess the activity. Diuretic effects in SHR and normotensive rats were observed in both the series of 10 and the 2- or 3-oxo derivatives (20 and 21). The relationship between the activities and the substituents on the phenyl ring is discussed.
一系列(取代苯基)-2, 3, 5, 6-四氢-1H-咪唑并[1, 2-a]咪唑(10)及其2-或3-氧代衍生物(20和21)被明确制备。这些化合物被评估了降压和利尿活性。在自发性高血压大鼠(SHR)中观察到化合物系列10具有降压活性,而化合物20和21不具备该活性。在SHR和正常血压大鼠中观察到系列10和2-或3-氧代衍生物(20和21)均具有利尿效果。讨论了活性与苯环上取代基之间的关系。